Abstract: The present invention provides compounds useful as inhibitors of Ca2+/calmodulin-dependent protein kinase (CaMKII), compositions thereof, and methods of using the same.

Abstract: Compounds according to Formulas I, IA or IB: to pharmaceutically acceptable composition, salts thereof, their synthesis and their use as SIK2 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and/or disorders such as cancer, stroke, cardiovascular, obesity and type II diabetes.

Abstract: The invention relates to compounds of Formula (I) wherein R1, R2, R3, R4 and R5 are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as modulators of the CXCR3 receptor.

Abstract: This invention relates to novel compounds which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of cancer.

Abstract: The present disclosure provides indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors of Formula I: or pharmaceutically acceptable salts thereof, in which X, L, n, m, R1, R2a, R2b, Rn, Rm, and Rt are as defined herein, as well as pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using the same to treat conditions mediated by IDO1.

Abstract: Generally, the present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.

Abstract: A method for producing an optically active ?-trifluoromethyl-?-amino acid derivative, the method including: allowing a compound represented by the following General Formula (1) and a compound represented by the following General Formula (2) to react in the presence of a copper-optically active phosphine complex obtained from a copper compound and an optically active phosphine compound, to thereby obtain an optically active ?-trifluoromethyl-?-amino acid derivative represented by the following General Formula (3):

Abstract: The compounds of formula (I) are inhibitors of SSAO activity wherein V, W, X, Y, Z, R1 and R2 are as defined in the claims.

Abstract: Provided herein are compounds and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of conditions associated with inhibition of HDAC (e.g., HDAC2).

Abstract: Provided herein are ergoline compounds and pharmaceutical compositions thereof. In some embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1A, 5-HT1B and 5-HT1D receptors without agonizing the 5-HT2B receptor using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the 5-HT2B adrenergic alpha2A and/or the alpha2B receptors using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the D2 and D3 receptor using the compounds and pharmaceutical compositions disclosed herein.

Abstract: The present invention provides compounds of Formula (V): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: Substituted dihydroisoxazole derivatives useful as inhibitors of ?-lactamases are provided. The invention further provides medical uses of substituted dihydroisoxazole derivatives, for example, as antibacterial agents.

Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.

Abstract: The present disclosure provides compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) have been found to bind bromodomains and/or bromodomain-containing proteins (e.g., bromo and extra terminal (BET) proteins). Also provided are methods, uses, and kits of the compounds and pharmaceutical compositions for inhibiting the activity (e.g., increased activity) of bromodomains and/or bromodomain-containing proteins and for treating and/or preventing in a subject diseases associated with bromodomains or bromodomain-containing proteins (e.g., proliferative diseases, cardiovascular diseases, viral infections, fibrotic diseases, neurological diseases, metabolic diseases, endocrine diseases, and radiation poisoning). The compounds, pharmaceutical compositions, and kits are also useful for male contraception.

Abstract: The present invention relates to the use of pteridines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to compounds per se and their use as medicines. The present invention also concerns processes for the preparation of such compounds, pharmaceutical compositions comprising them, and combinations of said compounds with other anti-HCV agents.

Abstract: Provided are compounds having formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as disclosed herein, or a pharmaceutically salt thereof. Pharmaceutical compositions comprising the compounds and methods of their use, for instance in treating senility, senile confusion, psychoses, psychoneuroses when anxiety and nervous tension were present, cerebral arteriosclerosis, nausea, depression, fatigue, debilitation, mild behavioral disorders, irritability, emotional instability, antisocial attitudes, anxiety, vertigo or incontinence, or symptom thereof, or in improving cognitive function in individuals, for instance, in individuals with Down syndrome and other conditions, are also provided.

Abstract: The present disclosure provides a compound of formula (I) and the use thereof for the therapeutic treatment of human cancers including B-cell lymphoma and autoimmune diseases such as rheumatoid arthritis, systemic lupus erythematosus, and multiple sclerosis.

Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as ERK (MAPK). Also provided are methods of using such compounds or compositions, and methods of using these compositions to modulate the activities of one or more of these kinases, especially for therapeutic applications such as the treatment disorders such as cancer.

Abstract: The present invention relates to Fused Tricyclic Heterocycle Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, X, Y, m, R1, R5, Ra and Rb are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocycle Derivative, and methods of using the Fused Tricyclic Heterocycle Derivatives for treating or preventing HIV infection in a subject.

Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.

Abstract: The present application relates to a new chlorin e6 derivatives and pharmaceutically acceptable salt thereof, as well as preparation and use thereof, which belongs to the medicine field. The chlorin e6 ether amino acid derivative comprises general structural formula I and optical isomers thereof. The preparation process comprises etherification of 3-vinyl in chlorin e6, A peptide is produced from 15-carboxylethyl and amino acid. The chlorin e6 ether amino acid derivative and pharmaceutically acceptable salt thereof can be used as a photodynamic anti-tumor drug. Compared with the prior similar photosensitizer Talaporfin used in clinic, the chlorin e6 ether amino acid derivative of the present application possess improved photodynamic anti-tumor activities and a high ratio of darktoxicity-phototoxicity.

Abstract: Stable crystalline forms of a compound represented by the formula (IA): an acid addition salt, and/or a solvate thereof are provided by the present invention. Said crystalline forms are extremely useful as materials for preparing medicines. Novel processes for preparing 6,7-unsaturated-7-carbamoyl morphinan derivatives are also provided by the present invention.

Abstract: The invention provides derivatives of cyclopamine having the following formula:

Abstract: The present invention relates spiro-cyclic amine derivatives of the formula (1) wherein R1; R2; R3; Q; —W-T-; R5; Z; and A have the definitions provided in the claims; or a pharmaceutically acceptable salt, a solvate or hydrate thereof or one or more N-oxides thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of diseases and conditions in which (a) S1P receptor (s) is (are) involved.

Abstract: The invention generally relates to novel fluorophore-labeled, bi- or multi-functional, chemically reactive and/or biologically active conjugates, and related compositions and methods thereof.

Abstract: The present application relates to novel 6-substituted indazoles having a carboxamide side chain, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of endometriosis, lymphomas, macular degeneration, COPD and psoriasis.

Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.

Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and neurological disorders, including, but not limited to, e.g., psychosis, schizophrenia, depression, movement disorders, and Parkinson's disease.

Abstract: The present invention provides fatty acid amide hydrolase inhibitors, solid forms thereof, compositions thereof, and methods of making and using the same.

Abstract: The present invention is a mono-functional branched organosiloxane compound that is liquid and shown by the following general formula (1) Ma-1MRa-2Db-1DRb-2Tc-1TRc-2Qd-1??(1) wherein M=R13SiO0.5, MR=R12R2SiO0.5, D=R12SiO, DR=R2R1SiO, T=R1SiO1.5, TR=R2SiO1.5, and Q=SiO2, where R1 represents a group selected from an alkyl group having 1 to 30 carbon atoms, and so on, R2 represents a hydrogen atom, and so on, a-1 represents an integer of 1 or more, b-1 and c-1 each represent an integer of 0 or more, and a-2, b-2, c-2, and d-1 each represent 0 or 1, provided that c-1, c-2, and d-1 are not simultaneously 0, a total of a-2, b-2, and c-2 is 1, and when b-1 is 0, a-1 is 2 or more and a total of c-1 and d-1 is 1 or more. There can be provided a novel mono-functional branched organosiloxane compound having a branched structure, and a method for producing the same.

Abstract: A tris[3-(alkoxysilyl)propyl] isocyanurate from the group of tris[3-(trialkoxysilyl)propyl] isocyanurate, tris[3-(alkyldialkoxysilyl)propyl] isocyanurate and tris[3-(dialkylalkoxysilyl)propyl] isocyanurate is prepared by hydrosilylation, by a) initially charging a mixture of at least one hydroalkoxysilane from the group of hydrotrialkoxysilane, hydroalkyldialkoxysilane, hydrodialkylalkoxysilane [called H-silane(s) for short] and a Pt catalyst, b) heating the mixture to a temperature of 40 to 170° C., c) then adding or metering in 1,3,5-triallyl-1,3,5-triazine-2,4,6(1H,3H,5H)-trione, at least one carboxylic acid and at least one alcohol as cocatalyst while mixing, and d) leaving the mixture to react and then working up the product mixture thus obtained.

Abstract: Methods, kits and devices for separating phospholipids and proteins from small molecules in biochemical samples can feature an apparatus having a wetting barrier, at least one fit and a separation media. For example, an apparatus can include at least one wall defining a chamber having an exit and an entrance; a wetting barrier disposed between the exit and entrance, so as to define a separation media space located between the wetting barrier and the exit and a sample receiving area located between the wetting barrier and the entrance; and a separation media disposed adjacent to the wetting barrier and having a specific affinity for phospholipids.

Abstract: The present invention relates to novel compounds that contain PNA units substituted with phosphonic acid ester functions or phosphonic acid functions, and have at least one chiral center. The compounds may be used for the treatment of viral diseases, such as AIDS.

Abstract: The following formula is an example of a phosphole compound of the present invention. The phosphole compound of the present invention has the characteristic of maintaining a high fluorescence quantum yield in a wide range of solvents from low-polarity solvents to high-polarity solvents, as well as the characteristic in which the fluorescence wavelength shifts to the longer wavelength side as the polarity of the solvent increases. Because of these characteristics, the phosphole compound of the present invention is expected to be used, for example, for quantitatively determining the polarity in the environment therearound by using the absorption wavelength and fluorescence wavelength thereof, or used as a new fluorescent probe dye or a highly efficient luminescent material in organic electronic devices.

Abstract: The present invention relates to monocrystalline metal organic frameworks comprising chromium ions and carboxylate ligands and the use of the same, for example their use for storing a gas. The invention also relates to methods for preparing metal organic frameworks comprising chromium, titanium or iron ions and carboxylate ligands. The methods of the invention allow such metal organic frameworks to be prepared in monocrystalline or polycrystalline forms.

Abstract: The present invention provides unimolecular metal complexes having increased activity in the copolymerization of carbon dioxide and epoxides. Also provided are methods of using such metal complexes in the synthesis of polymers. According to one aspect, the present invention provides metal complexes comprising an activating species with co-catalytic activity tethered to a multidentate ligand that is coordinated to the active metal center of the complex.

Abstract: With the rise in resistance to antibiotics such as methicillin, there is a need for new drugs. The invention provides small molecules that inhibit cellular drug targets such as UPPS and FPPS by interacting with binding pockets, thereby preventing enzyme function. Compounds described herein are also active against Staphylococcus aureus (MIC90˜0.25 ?g/mL), can potently synergize with methicillin (fractional inhibitory concentration index=0.25), and are protective in a mouse infection model. The invention therefore provides numerous compounds for anti-bacterial treatments and for restoring sensitivity to drugs such as methicillin, using combination therapies.

Abstract: Provided herein are processes for the preparation of 5-azacytidine, useful for treating, preventing, and/or managing diseases or conditions including cancer, disorders related to abnormal cell proliferation, hematologic disorders, and myelodysplastic syndromes (MDS), wherein 5-azacytidine is represented by the structure:

Abstract: The present invention provides novel stabilized crosslinked compounds having secondary structure motifs, libraries of these novel compounds, and methods for the synthesis of these compounds libraries thereof. The synthesis of these novel stabilized compounds involves (1) synthesizing a peptide from a selected number of natural or non-natural amino acids, wherein the peptide comprises at least two moieties capable of undergoing reaction to promote carbon-carbon bond formation; and (2) contacting the peptide with a reagent to generate at least one crosslinker and to effect stabilization of a secondary structure motif. The present invention, in a preferred embodiment, provides stabilized p53 donor helical peptides. Additionally, the present invention provides methods for disrupting the p53/MDM2 binding interaction comprising (1) providing a crosslinked stabilized ?-helical structure; and (2) contacting the crosslinked stabilized ?-helical structure with MDM2.

Abstract: A method for separating and purifying recombinant human serum albumin (rHSA) from transgenic rice grain, sequentially comprising the steps of: 1) subjecting crude extract of rHSA to cation exchange chromatography to obtain primary product I; 2) subjecting the primary product I to anion exchange chromatography to obtain secondary product II; 3) subjecting the secondary product II to hydrophobic chromatography to obtain purified rHSA. The method may further comprise a step of ceramic hydroxyapatite chromatography prior to the hydrophobic chromatography. The method has the advantages of low cost and easy operation. The resultant rHSA has a purity of about 99% by HPLC.

Abstract: Novel compositions for removing impurities such as, protein aggregates, from a sample containing a protein of interest, e.g., an antibody. Such compositions can be used prior to the virus filtration step during protein purification, to remove aggregates and protect the virus filter from fouling, therefore improving virus filter capacity. A porous solid support including a co-polymer having at least two monomers, wherein at least one of the monomers comprises acrylamide and at least a second monomer comprises a hydrophobic binding group, where the solid support selectively binds protein aggregates, thereby to separate the monomeric protein of interest from the protein aggregates. The method can be performed under neutral to high pH and high conductivity conditions.

Abstract: An isolated peptide or fusion having the peptide useful to interfere with the phosphorylation of Nox1, block or inhibit binding of NoxA1 activation domain (AD) to Nox1, and/or prevent or inhibit assembly of the p47phox/NoxA1 complex with Nox1, or a vector encoding the peptide or fusion thereof, and methods of using the peptide, fusion or vector are provided.

Abstract: There is described a material comprising tapes, ribbons, fibrils or fibers characterized in that each of the ribbons, fibrils or fibers have an antiparallel arrangement of peptides in a ?-sheet tape-like substructure.

Abstract: We describe peptides and their uses for the treatment of autoimmune, inflammatory and metabolic diseases.

Abstract: Methods and compositions related to the selective, specific disruption of multiple ligand-receptor signaling interactions, such as ligand-receptor interactions implicated in disease, are disclosed. These interactions may involve multiple cytokines in a single receptor family or multiple ligand receptor interactions from at least two distinct ligand-receptor families. The compositions may comprise polypeptides having composite sequences that comprise sequence fragments of two or more ligand binding sites. The methods and compositions may involve sequence fragments of two or more ligand binding sites that are arranged to conserve the secondary structure of each of the ligands from which the sequence fragments were taken.

Abstract: Fusion proteins comprising a portion of the HIV-1 Env protein (gp120 and gp140) and single-chain fragment V regions (ScFv) of an enhancing antibody that exhibits binding specificity for HIV-1 Env protein are disclosed that may serve in immunogenic formulations for vaccination against HIV-1 infection, as well as methods of generating an immune response using the fusion proteins.

Abstract: The invention relates to compositions of vault complexes containing recombinant membrane lytic proteins, such as an adenovirus protein VI lytic domain, and methods of using the vault complexes to facilitate delivery and entry of a biomolecule into a cell or subject.

Abstract: A general method and strains of bacteria are described by means where the endogenous DNAK protein or homolog of the DNAK protein is tagged with a recognizable amino acid sequence and that through this tag, DNAK may be efficiently removed, and as such, recombinant protein purification may be greatly improved both in yield and purity with simplified purification steps that remove the DNAK and reduced cost, waste accumulation and labor, and the isolated recombinant protein will significantly benefit research and therapeutics in its application.

Abstract: The present invention provides proteins that are suitable to be used as the active ingredient in subunit vaccine against Mycoplasma spp. The present invention also provides a subunit vaccine made therefrom. Said proteins have been experimentally proved to have the capability of inducing sufficient immune response to avoid pigs from Mycoplasma spp. infection. Said vaccine may have one of said proteins as active ingredient; or may have two or more of said proteins and is formulated as a cocktail vaccine. The present vaccine not only is safer than the conventional vaccines but also has equal or even better immune efficiency than the conventional ones. Furthermore, fusion partners suitable for producing said proteins of high solubility are also proved, which can significantly reduce production cost.

Abstract: The invention provides short peptides derived from an insect neuropeptide for controlling insects, particularly peptides or their analogs derived from PBAN family neuropeptide having at least one dPhe residue. The invention further provides an environmentally friendly method for controlling and/or preventing insect infestation by applying the short peptides in very low concentrations.